Detailed Analysis of the Scope and Claims of United States Patent 7,815,942
Introduction
United States Patent 7,815,942, titled "Rasagiline Formulations of Improved Content Uniformity," is a significant patent in the pharmaceutical industry, particularly for the treatment of Parkinson's disease. This patent, assigned to Teva Pharmaceutical Industries, Ltd., focuses on formulations of the enantiomer R(+)-N-propargyl-1-aminoindan, known as rasagiline.
Background of the Invention
Rasagiline is a selective, irreversible inhibitor of the B-form of the enzyme monoamine oxidase (MAO-B), which is crucial for the treatment of Parkinson's disease. The patent builds upon earlier disclosures, such as U.S. Pat. No. 5,532,415, which introduced R(+)-N-propargyl-1-aminoindan and its preparation methods[1].
Summary of the Invention
The primary objective of this patent is to enhance the content uniformity of solid pharmaceutical compositions containing rasagiline. The inventors discovered that specific particle size distributions of rasagiline particles significantly improve the uniformity of the drug content. This is achieved through milling or other methods to alter the particle size distribution (PSD) of rasagiline, ensuring greater uniformity in the drug product[1].
Scope of the Invention
Particle Size Distribution (PSD)
The patent emphasizes the importance of PSD in achieving content uniformity. By milling rasagiline particles to reduce their size, the inventors were able to meet stringent content uniformity standards set by regulatory bodies such as the United States Pharmacopeia (USP). The USP requires a multi-stage content uniformity test, including assaying ten tablets to ensure a relative standard deviation (RSD) of active content less than or equal to 6.0% and no value outside 85-115%, and further assaying twenty more tablets to ensure the RSD for all thirty tablets is less than or equal to 7.8%, with no more than one value outside 85-115% and no value outside 75-125% of stated content[1].
Manufacturing Process
The patent details various methods for altering the PSD of rasagiline, including milling, which is a critical step in ensuring the uniform distribution of the active ingredient in the final drug product. This process is essential for maintaining the efficacy and safety of the medication.
Claims of the Patent
The patent includes several claims that define the scope of the invention:
Claim 1
The first claim typically defines the broadest scope of the invention, which in this case involves a pharmaceutical composition comprising rasagiline particles with a specific PSD to ensure content uniformity.
Claim 2-10
Subsequent claims narrow down the scope by specifying different aspects of the invention, such as the method of preparing the rasagiline particles, the range of particle sizes, and the formulation of the drug product. These claims provide a detailed description of how to achieve the improved content uniformity[1].
Patent Landscape
Related Patents and Applications
The patent is part of a larger family of patents and applications related to rasagiline formulations. Other related applications include provisional applications No. 60/720,908 and No. 60/655,622, filed on September 27, 2005, and February 23, 2005, respectively. These applications and subsequent filings contribute to the comprehensive protection of the invention[1].
Exclusivity and Therapeutic Equivalence
The patent's exclusivity and therapeutic equivalence are documented in resources like the FDA's Orange Book. This book provides information on the therapeutic equivalence of drug products, including those containing rasagiline, and lists the patents and exclusivity periods associated with these products[2].
Patent Analytics and Strategic Importance
Claim Coverage and Scope Concepts
Patent analytics tools, such as those described by Schwegman, can help in understanding the claims and scope concepts of this patent. These tools categorize patents by claims and overarching scope concepts, enabling a more efficient analysis of the patent landscape. This is particularly useful for identifying gaps in coverage and future design opportunities[3].
Core Patent Analysis
Using patent intelligence systems like Xlpat, researchers can analyze the core patents in the field of drug formulations, including those related to rasagiline. This analysis helps in identifying key patents, their citation frequency, and their impact on the R&D landscape, guiding future investment and research initiatives[4].
Practical Implications
Regulatory Compliance
The improved content uniformity achieved through this patent ensures compliance with stringent regulatory standards, which is crucial for the approval and marketing of pharmaceutical products.
Patient Safety and Efficacy
Uniform drug content is vital for patient safety and the efficacy of the medication. This patent contributes significantly to ensuring that patients receive consistent doses of rasagiline, which is essential for managing Parkinson's disease effectively.
Key Takeaways
- Improved Content Uniformity: The patent focuses on achieving better content uniformity in rasagiline formulations through specific particle size distributions.
- Manufacturing Process: Milling and other methods are used to alter the PSD of rasagiline particles.
- Regulatory Compliance: The invention meets USP standards for content uniformity.
- Patent Landscape: Part of a broader family of patents and applications related to rasagiline formulations.
- Strategic Importance: Essential for ensuring patient safety and efficacy, and for compliance with regulatory standards.
FAQs
What is the main objective of United States Patent 7,815,942?
The main objective is to improve the content uniformity of solid pharmaceutical compositions containing rasagiline through specific particle size distributions.
How is content uniformity achieved in this patent?
Content uniformity is achieved by milling or other methods to reduce the particle size of rasagiline, ensuring a uniform distribution of the active ingredient.
What regulatory standards does this patent comply with?
The patent complies with the content uniformity standards set by the United States Pharmacopeia (USP).
Why is content uniformity important in pharmaceuticals?
Content uniformity is crucial for patient safety and the efficacy of the medication, ensuring that patients receive consistent doses of the active ingredient.
How does this patent fit into the broader patent landscape?
It is part of a family of patents and applications related to rasagiline formulations and is documented in resources like the FDA's Orange Book.
Sources
- United States Patent and Trademark Office. Rasagiline Formulations of Improved Content Uniformity. US 7,815,942 B2.
- FDA Orange Book. Approved Drug Products with Therapeutic Equivalence Evaluations.
- Schwegman, Lundberg & Woessner, P.A. Patent Analytics.
- Scientific Research Publishing. Analysis of Drug Patent in American Universities Based on Xlpat.
